Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics

Expert Opin Investig Drugs. 2010 Jan;19(1):27-43. doi: 10.1517/13543780903483191.


Importance of the field: The Polo-like kinase (Plk) family has emerged as an important regulator in cell cycle progression. Plks belong to a family of serine/threonine kinases and exist in four isoforms Plk1- 4. However, only one of these isoforms, Plk1, is shown to be involved in the activation of Cdc2, chromosome segregation, centrosome maturation, bipolar spindle formation and execution of cytokinesis. The activity of Plk1 is elevated in tissues and cells with a high mitotic index. In patients, Plk1 is overexpressed in tumors including those derived from lung, breast, colon, pancreas, prostate and ovary. Plk1 depletion is associated with the decrease in cell viability and induction of apoptosis in various cancerous cells. Several Plk1 inhibitors are in different phases of clinical development for anticancer therapy.

Areas covered in this review: The focus of present review is to highlight Plk1 as a promising therapeutic approach for the treatment of cancer. The review discusses the role of Plk1 in cancer and the current status of Plk1 inhibitors, as well as highlighting the possible beneficial effect of inhibition of Plk1 as compared to other mitotic targets.

What the reader will gain: Readers will get a comprehensive overview of Plk1 as a novel anticancer drug target. This review will also update readers about the progress made in the field of Plk1 inhibitors.

Take home message: The current literature about Plk1 inhibitors and knockout studies favor Plk1 inhibition as a potential antitumor therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Cell Cycle Proteins / antagonists & inhibitors*
  • Cell Cycle Proteins / biosynthesis
  • Cell Cycle Proteins / chemistry
  • Clinical Trials as Topic
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / pathology
  • Protein-Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein-Serine-Threonine Kinases / biosynthesis
  • Protein-Serine-Threonine Kinases / chemistry
  • Proto-Oncogene Proteins / antagonists & inhibitors*
  • Proto-Oncogene Proteins / biosynthesis
  • Proto-Oncogene Proteins / chemistry


  • Antineoplastic Agents
  • Cell Cycle Proteins
  • Proto-Oncogene Proteins
  • Protein-Serine-Threonine Kinases
  • polo-like kinase 1